Invention Grant
- Patent Title: Biologically active macrolides, compositions, and uses thereof
- Patent Title (中): 生物活性大环内酯类,组合物及其用途
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Application No.: US12851691Application Date: 2010-08-06
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Publication No.: US08741947B2Publication Date: 2014-06-03
- Inventor: Michael R. Boyd , Kirk R. Gustafson , Charles L. Cantrell
- Applicant: Michael R. Boyd , Kirk R. Gustafson , Charles L. Cantrell
- Applicant Address: US DC Washington
- Assignee: The United States of America, as represented by the Secretary of the Department of Health and Human Services
- Current Assignee: The United States of America, as represented by the Secretary of the Department of Health and Human Services
- Current Assignee Address: US DC Washington
- Agency: Leydig, Voit & Mayer, Ltd.
- Main IPC: A01N43/02
- IPC: A01N43/02 ; A61K31/335 ; C07D309/00

Abstract:
The present invention provides a compound of the formula (I) or (II, wherein R1 is H, alkyl, alkenyl or aryl, R2 is H, alkyl or aryl, R3 is H, a alkyl, alkenyl or aryl, R4 and R4-R8 are independently R10, C(O)R10 or SO2R10, wherein R10 is H, alkyl, alkenyl or aryl, and R9 is R9a, C(O)R9a or SO2R9a, wherein R9a is H, alkyl, alkenyl or aryl. R9a can be unsubstituted or substituted with one or more oxo(═O), OR9b, OC(O)R9b, OSO2R9b, NHR9b, NHC(O)R9b and NHSO2R9b groups. R9b is H, alkyl, alkenyl, or aryl. R9b can be unsubstituted or substituted with one or more groups such as oxo(═O), OR9c, CO2R9c, CO2R9c and OC(O)R9c. R9c is H, or a unsubstituted or substituted alkyl, alkenyl or aryl. The present invention further provides a composition comprising at least one compound of the present invention and a pharmaceutically acceptable carrier, alone or in combination with at least one additional active agent. The present invention further provides a method of treating a condition treatable by the inhibition of vacuolar-type (H+)-ATPase and a method of treating cancer.
Public/Granted literature
- US20100298248A1 BIOLOGICALLY ACTIVE MACROLIDES, COMPOSITIONS, AND USES THEREOF Public/Granted day:2010-11-25
Information query
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